SAN DIEGO--(BUSINESS WIRE)--Jun 6, 2011 - Ligand
Pharmaceuticals Incorporated (NASDAQ:LGND) today announced that
interim data from a Phase IIa study with its Captisol-enabled,
propylene glycol-free, Melphalan program was featured today in a
poster presentation at the 2011 American Society of Clinical
Oncology (ASCO) Annual Meeting in Chicago, June 3-7, 2011.

This Phase IIa study compared the safety, tolerability, and
pharmacokinetic profiles of a new propylene glycol-free Melphalan
intravenous formulation and the current clinically used intravenous
formulation of Melphalan (sold as Alkeran®) for multiple
myeloma patients undergoing autologous transplantation. This
Captisol-enabled product is expected to allow for longer
administration durations and slower infusion rates, potentially
enabling clinicians to safely achieve a higher dose intensity of
pre-transplant chemotherapy.

The key findings presented on the poster include:

All patients achieved myeloablation
followed by successful engraftment

Except for expected grade 2-3
toxicities related to high dose Melphalan, no additional toxicities
were reported

PK analysis revealed that the new
propylene glycol-free Melphalan met the requirements for
establishment of bioequivalence to Alkeran

Based on these preliminary results from
the Phase IIa, the follow-on study (Phase IIb) will utilize a
dosing regimen that appears to be comparable to Alkeran. This study
will be designed to expose patients exclusively to the propylene
glycol-free formulation and will further elaborate safety and
efficacy measures for the new product

The poster presentation can be viewed by visiting the Investor
Relations section of Ligand's Web site at
www.ligand.com.

“The data presented today help build a strong case that
this new Captisol-enabled formulation of Melphalan could be a
significant improvement over the standard of care for patients
going through myeloablation,” said Dr. Omar Aljitawi from the
University of Kansas Medical Center and Principal Investigator for
this study. “The ability to remove propylene glycol from the
formulation and extend stability in solution, all while improving
drug exposure in patients, should be meaningful to the clinicians
treating these patients,” added Dr. Aljitawi.

“This data clearly sets the stage for a pivotal safety
study to be performed allowing us to bring this program to the NDA
filing stage relatively quickly,” said John Higgins,
President and Chief Executive Officer of Ligand Pharmaceuticals.
“While the Captisol-enabled pipeline that we acquired
recently with our acquisition of CyDex has several valuable
programs, we viewed the Melphalan program as one of the most
advanced and exciting. The recent acquisition of the
Captisol-enabled Nexterone program by Baxter, along with our just
announced deal with The Medicines Company for Captisol-enabled,
rapid-onset Clopidogrel, demonstrate the clear opportunity that
these reformulations of existing products represent.”

About Melphalan

Melphalan HCl for Injection (Propylene Glycol-Free), a
reformulation of Alkeran for Injection, incorporates the
Captisol® brand of Î²-cyclodextrin sulfobutyl
ethers, sodium salts (also known as [SBE]7m-Î²-CD) into
a freeze-dried product developed by CyDex Pharmaceuticals, Inc.
(CyDex). This product is reconstituted and further diluted with
normal saline. Captisol improves stability allowing for longer
administration durations, slower infusion rates and potentially
could enable safe administration of higher doses of Melphalan, and
lead to better therapeutic outcomes, which may also permit reaching
a wider patient population and use in a number of other lymphoma
and leukemia diseased populations that indicate ASCT as treatment
modality.

About Ligand Pharmaceuticals

Ligand is a biopharmaceutical company with a business model that
is based upon the concept of developing or acquiring royalty
revenue generating assets and coupling them to a lean corporate
cost structure. Ligand's goal is to produce a bottom line that
supports a sustainably profitable business. By diversifying the
portfolio of assets across numerous technology types, therapeutic
areas, drug targets, and industry partners, we offer investors an
opportunity to invest in the increasingly complicated and
unpredictable pharmaceutical industry. In comparison to its peers,
we believe Ligand has assembled one of the largest and most
diversified asset portfolios in the industry with the potential to
generate revenue in the future. These therapies address the unmet
medical needs of patients for a broad spectrum of diseases
including hepatitis, muscle wasting, Alzheimer's disease,
dyslipidemia, diabetes, anemia, COPD, asthma, rheumatoid arthritis
and osteoporosis. Ligand has established multiple alliances with
the world's leading pharmaceutical companies including
GlaxoSmithKline, The Medicines Company, Pfizer, Bristol-Myers
Squibb and AstraZeneca. For more information, please visit
www.ligand.com. Follow Ligand on Twitter @Ligand_LGND.

Caution Regarding Forward-Looking Statements

This news release contains forward-looking statements by Ligand
that involve risks and uncertainties and reflect Ligand's judgment
as of the date of this release. These statements include those
related to clinical trials of Captisol-enabled Melphalan's profile,
market size and possibility of commercial success, efficacy,
potency, competitiveness, and the strength of Ligand's product
portfolio. Actual events or results may differ from our
expectations. For example, there can be no assurance that
Captisol-enabled Melphalan and Alkeran or other potential
Captisol-enabled drugs will progress through clinical development
or receive required regulatory approvals within the expected time
lines or at all, that further clinical trials will confirm any
safety or other characteristics or profile described in this press
release, that there will be a market of any size for
Captisol-enabled Melphalan, or that Captisol-enabled Melphalan will
be beneficial to patients or successfully marketed. Additional
information concerning these and other risk factors affecting
Ligand can be found in prior press releases as well as in public
periodic filings with the Securities and Exchange Commission,
available via
www.ligand.com. Ligand disclaims any intent or obligation to
update these forward-looking statements beyond the date of this
release. This caution is made under the safe harbor provisions of
the Private Securities Litigation Reform Act of 1995.

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